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Coluracetam 135463-81-9 Coluracetam Research Grade ≥98%
Brief Introduction
Brief Introduction
Coluracetam (development codes: MKC-231, BCI-540) is a newly synthesized tetrahydrofuroquinoline analogue and a member of a novel class of nootropic agents . Unlike traditional racetam compounds, Coluracetam exerts its effects by enhancing high-affinity choline uptake (HACU) , the rate-limiting step for acetylcholine synthesis . This unique mechanism of action makes it particularly valuable in research on cholinergic dysfunction-related disorders such as Alzheimer's disease.
Key Scientific Value & Findings
Unique Choline Uptake Enhancement Mechanism: Coluracetam is a new choline uptake enhancer . MKC-231 significantly increased high-affinity choline uptake when incubated with hippocampal synaptosomes of ethylcholine mustard aziridinium ion (AF64A)-treated rats, but not of normal rats . Studies show that MKC-231 increased the Vmax of HACU and Bmax of [3H]-HC-3 binding by 1.6 and 1.7-fold, respectively . In [3H]-MKC-231 binding and Biacore analysis, MKC-231 showed noticeable affinity for cloned high-affinity choline transporters (CHT1) .
No Effect on Acetylcholinesterase or Receptors: MKC-231 did not affect AChE activity, [3H]-quinuclidinyl benzilate binding, or [3H]-pirenzepine binding , indicating its mechanism is completely distinct from acetylcholinesterase inhibitors or direct cholinergic agonists .
Persistent Improvement with Chronic Administration: In chronic experiments, MKC-231 (0.3, 1.0, or 3.0 mg/kg p.o., once daily for 11 days) significantly improved working memory deficits induced by AF64A in mice . Correct response rates in a delayed non-matching to sample task in a T-maze improved from 61.1% (AF64A+vehicle) to 86.1%, 85.0%, and 83.3% at doses of 0.3, 1.0, and 3.0 mg/kg, respectively . Acute single administration (same doses) did not significantly improve AF64A-induced working memory deficits .
Restoration of Hippocampal ACh Levels: Chronic oral administration of MKC-231 (0.3 and 1.0 mg/kg, once daily for 12 days) significantly reversed the depletion of hippocampal ACh content induced by AF64A in mice . ACh levels increased from 60.8% of control (AF64A+vehicle) to 84.4% and 75.5% of control at doses of 0.3 and 1.0 mg/kg, respectively . The effect at 3.0 mg/kg (65.0% of control) was not significant, indicating a bell-shaped dose-response curve . Acute oral administration of MKC-231 did not reverse AF64A-induced hippocampal ACh depletion .
Improvement of Water Maze Learning Deficits: Oral administration of MKC-231 (1-10 mg/kg) significantly improved learning deficits in the Morris water maze of AF64A-treated rats . Unlike high doses of tacrine, MKC-231 did not produce any significant side effects like tremor, salivation, or hypothermia .
Modulation of Glutamate and GABA Levels: Coluracetam also acts by increasing glutamate and GABA levels, neurotransmitters involved in learning and memory . Additionally, it increases the efficiency of signal transmission between neurons
Our Supply & Service Advantages
Our Supply & Service Advantages
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Stable Supply, Consistent Quality: Leveraging robust Chinese manufacturing resources, we ensure stable delivery of bulk orders with consistent quality across all batches.
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